Pharmaceutical dopamine glycoconjugate compositions and methods of their preparation and use

Abstract

Hydrophilic transportable N-linked glycosyl dopaminergic prodrug compounds and methods of their use.

I claim: 
     
       1. A pharmaceutical composition comprising
 an agent selected from the group consisting of an additive, a stabilizer, a carrier, a binder, a buffer, an excipient, an emollient, a disintegrant, a lubricating agent, an antimicrobial agent and a preservative and 
 a compound having the formula: 
 
       
         
           
           
               
               
           
         
          wherein:
 Ring 1 is a substituted aryl ring; 
 X and Y are carbon atoms; 
 R 0  is hydrogen; 
 R 3  is hydroxyl; 
 N is the nitrogen atom of an amine or an amide; 
 R 1 , R 4 , R 5 , R 5′ , R 6 , R 6′  and R 7  are hydrogen, 
 R 2  is hydroxyl, 
 z is a carbon atom, 
 E is a residue of a straight chain hexose sugar, 
 or a pharmaceutically acceptable salt thereof. 
 
       
     
     
       2. The pharmaceutical composition of  claim 1 , wherein E is a sugar residue having a structure: 
       
         
           
           
               
               
           
         
       
     
     
       3. A pharmaceutical composition comprising
 an agent selected from the group consisting of an additive, a stabilizer, a carrier, a binder, a buffer, an excipient, an emollient, a disintegrant, a lubricating agent, an antimicrobial agent and a preservative and 
 a dopamine ribonamide or a pharmaceutically acceptable salt thereof. 
 
     
     
       4. A pharmaceutical composition comprising
 an agent selected from the group consisting of an additive, a stabilizer, a carrier, a binder, a buffer, an excipient, an emollient, a disintegrant, a lubricating agent, an antimicrobial agent and a preservative and 
 a dopamine amide, wherein the dopamine amide is produced by a process comprising:
 a) reacting a lactone of a sugar and 3-hydroxytyramine, and 
 b) collecting the dopamine amide, 
 wherein the reaction yields a sugar residue having a structure: 
 
 
       
         
           
           
               
               
           
         
       
     
     
       5. A process for preparing the pharmaceutical composition of  claim 1 , comprising:
 reacting a lactone of a sugar and an optionally substituted phenethylamine, and 
 collecting the phenethylamide. 
 
     
     
       6. A process of preparing the pharmaceutical composition of  claim 4 , comprising
 reacting a lactone of a sugar and 3-hydroxytyramine, and 
 collecting the dopamine amide. 
 
     
     
       7. A method of ameliorating Parkinson's Disease in a subject in need thereof comprising administering to the subject the pharmaceutical composition of  claim 1 . 
     
     
       8. A method for ameliorating Parkinson's Disease in a subject in need thereof, comprising administering to the subject a pharmaceutical composition of  claim 3 . 
     
     
       9. A method for ameliorating Parkinson's Disease in a subject in need thereof, comprising administering to the subject a pharmaceutical composition of  claim 4 .